Hybrid Nanobeads for Oral Indomethacin Delivery

The oral administration of the anti-inflammatory indomethacin (INDO) causes severe gastrointestinal side effects, which are intensified in chronic inflammatory conditions when a continuous treatment is mandatory. The development of hybrid delivery systems associates the benefits of different (nano)...

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Main Authors: Flávia Monique Rocha Bonetti, Eneida de Paula, Belchiolina Beatriz Fonseca, Gabriela Ribeiro da Silva, Leandro Santana Soares da Silva, Ludmilla David de Moura, Márcia Cristina Breitkreitz, Gustavo Henrique Rodrigues da Silva, Lígia Nunes de Morais Ribeiro
Format: Article
Language:English
Published: MDPI AG 2022-03-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/14/3/583
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author Flávia Monique Rocha Bonetti
Eneida de Paula
Belchiolina Beatriz Fonseca
Gabriela Ribeiro da Silva
Leandro Santana Soares da Silva
Ludmilla David de Moura
Márcia Cristina Breitkreitz
Gustavo Henrique Rodrigues da Silva
Lígia Nunes de Morais Ribeiro
author_facet Flávia Monique Rocha Bonetti
Eneida de Paula
Belchiolina Beatriz Fonseca
Gabriela Ribeiro da Silva
Leandro Santana Soares da Silva
Ludmilla David de Moura
Márcia Cristina Breitkreitz
Gustavo Henrique Rodrigues da Silva
Lígia Nunes de Morais Ribeiro
author_sort Flávia Monique Rocha Bonetti
collection DOAJ
description The oral administration of the anti-inflammatory indomethacin (INDO) causes severe gastrointestinal side effects, which are intensified in chronic inflammatory conditions when a continuous treatment is mandatory. The development of hybrid delivery systems associates the benefits of different (nano) carriers in a single system, designed to improve the efficacy and/or minimize the toxicity of drugs. This work describes the preparation of hybrid nanobeads composed of nanostructured lipid carriers (NLC) loading INDO (2%; <i>w</i>/<i>v</i>) and chitosan, coated by xanthan. NLC formulations were monitored in a long-term stability study (25 °C). After one year, they showed suitable physicochemical properties (size < 250 nm, polydispersity < 0.2, zeta potential of −30 mV and spherical morphology) and an INDO encapsulation efficiency of 99%. The hybrid (lipid-biopolymers) nanobeads exhibited excellent compatibility between the biomaterials, as revealed by structural and thermodynamic properties, monodisperse size distribution, desirable in vitro water uptake and prolonged in vitro INDO release (26 h). The in vivo safety of hybrid nanobeads was confirmed by the chicken embryo (CE) toxicity test, considering the embryos viability, weights of CE and annexes and changes in the biochemical markers. The results point out a safe gastro-resistant pharmaceutical form for further efficacy assays.
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spelling doaj.art-970fd11fd767432cac8cdb9f6244d57b2023-11-30T21:56:59ZengMDPI AGPharmaceutics1999-49232022-03-0114358310.3390/pharmaceutics14030583Hybrid Nanobeads for Oral Indomethacin DeliveryFlávia Monique Rocha Bonetti0Eneida de Paula1Belchiolina Beatriz Fonseca2Gabriela Ribeiro da Silva3Leandro Santana Soares da Silva4Ludmilla David de Moura5Márcia Cristina Breitkreitz6Gustavo Henrique Rodrigues da Silva7Lígia Nunes de Morais Ribeiro8Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas—UNICAMP, Campinas 13083-862, SP, BrazilDepartment of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas—UNICAMP, Campinas 13083-862, SP, BrazilSchool of Veterinary Medicine, Federal University of Uberlândia—UFU, Uberlândia 38410-337, MG, BrazilSchool of Veterinary Medicine, Federal University of Uberlândia—UFU, Uberlândia 38410-337, MG, BrazilSchool of Veterinary Medicine, Federal University of Uberlândia—UFU, Uberlândia 38410-337, MG, BrazilDepartment of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas—UNICAMP, Campinas 13083-862, SP, BrazilDepartment of Analytical Chemistry, Institute of Chemistry, University of Campinas—UNICAMP, Campinas 13083-970, SP, BrazilDepartment of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas—UNICAMP, Campinas 13083-862, SP, BrazilDepartment of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas—UNICAMP, Campinas 13083-862, SP, BrazilThe oral administration of the anti-inflammatory indomethacin (INDO) causes severe gastrointestinal side effects, which are intensified in chronic inflammatory conditions when a continuous treatment is mandatory. The development of hybrid delivery systems associates the benefits of different (nano) carriers in a single system, designed to improve the efficacy and/or minimize the toxicity of drugs. This work describes the preparation of hybrid nanobeads composed of nanostructured lipid carriers (NLC) loading INDO (2%; <i>w</i>/<i>v</i>) and chitosan, coated by xanthan. NLC formulations were monitored in a long-term stability study (25 °C). After one year, they showed suitable physicochemical properties (size < 250 nm, polydispersity < 0.2, zeta potential of −30 mV and spherical morphology) and an INDO encapsulation efficiency of 99%. The hybrid (lipid-biopolymers) nanobeads exhibited excellent compatibility between the biomaterials, as revealed by structural and thermodynamic properties, monodisperse size distribution, desirable in vitro water uptake and prolonged in vitro INDO release (26 h). The in vivo safety of hybrid nanobeads was confirmed by the chicken embryo (CE) toxicity test, considering the embryos viability, weights of CE and annexes and changes in the biochemical markers. The results point out a safe gastro-resistant pharmaceutical form for further efficacy assays.https://www.mdpi.com/1999-4923/14/3/583NLChybrid nanobeadbiopolymersanti-inflammatorychicken embryo model
spellingShingle Flávia Monique Rocha Bonetti
Eneida de Paula
Belchiolina Beatriz Fonseca
Gabriela Ribeiro da Silva
Leandro Santana Soares da Silva
Ludmilla David de Moura
Márcia Cristina Breitkreitz
Gustavo Henrique Rodrigues da Silva
Lígia Nunes de Morais Ribeiro
Hybrid Nanobeads for Oral Indomethacin Delivery
Pharmaceutics
NLC
hybrid nanobead
biopolymers
anti-inflammatory
chicken embryo model
title Hybrid Nanobeads for Oral Indomethacin Delivery
title_full Hybrid Nanobeads for Oral Indomethacin Delivery
title_fullStr Hybrid Nanobeads for Oral Indomethacin Delivery
title_full_unstemmed Hybrid Nanobeads for Oral Indomethacin Delivery
title_short Hybrid Nanobeads for Oral Indomethacin Delivery
title_sort hybrid nanobeads for oral indomethacin delivery
topic NLC
hybrid nanobead
biopolymers
anti-inflammatory
chicken embryo model
url https://www.mdpi.com/1999-4923/14/3/583
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